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新型单胺氧化酶抑制剂:专利研究综述(2012-2014)。

Novel monoamine oxidase inhibitors: a patent review (2012 - 2014).

机构信息

Sapienza University of Rome, Department of Drug Chemistry and Technologies , P.le A. Moro 5, 00185, Rome , Italy +39 06 49913149 ; +39 06 49913923 ;

出版信息

Expert Opin Ther Pat. 2015 Jan;25(1):91-110. doi: 10.1517/13543776.2014.982535. Epub 2014 Nov 15.

Abstract

INTRODUCTION

Monoamine oxidase (MAO) inhibitors, despite the initial pharmacological interest, are used in clinic for their antidepressant effect and in the management of Parkinson symptoms, due to the established neuroprotective action. Efficacy and tolerability emerged from large-scale and randomized clinical trials.

AREAS COVERED

Thirty-six patents range from April 2012 to September 2014. The number of chemotypes with inhibitory effects on MAO is truly high (40 synthetic compounds, 22 natural products and 6 plant extracts reported and licensed), and the present review is comprehensive of all compounds, which have been patented for their relevance to clinical medicine in this period range (27 patents). Moreover, some of the collected patents deal with new formulations of compounds endowed with MAO inhibitory properties (two patents) and new therapeutic options/drug associations for already known MAO inhibitors (seven patents).

EXPERT OPINION

The patents reported in this review showed that the interest in this field is constant and mainly devoted to the study of selective MAO-B inhibitors, used as drugs for the treatment of neurological disorders. The development of novel human MAO inhibitors took advantage of the discovery of new therapeutic targets (cancer, hair loss, muscle dystrophies, cocaine addiction and inflammation), the recognized role of MAOs as molecular biomarkers and their activity in other tissues.

摘要

简介

单胺氧化酶(MAO)抑制剂最初在药理学上引起关注,后来因其抗抑郁作用和在帕金森症状管理中的作用而在临床上得到应用,这是因为其具有明确的神经保护作用。其疗效和耐受性是通过大规模随机临床试验确定的。

涵盖领域

涵盖了 2012 年 4 月至 2014 年 9 月的 36 项专利。具有 MAO 抑制作用的化学型数量非常多(报道和授权的 40 种合成化合物、22 种天然产物和 6 种植物提取物),本综述涵盖了这一时期所有与临床医学相关的化合物专利(27 项)。此外,收集的一些专利涉及具有 MAO 抑制特性的化合物的新配方(两项专利)和已有的 MAO 抑制剂的新治疗选择/药物联合(七项专利)。

专家意见

本综述中报道的专利表明,人们对这一领域的兴趣持续不减,主要致力于研究选择性 MAO-B 抑制剂,将其作为治疗神经紊乱的药物。新型人 MAO 抑制剂的开发利用了新的治疗靶点(癌症、脱发、肌肉萎缩症、可卡因成瘾和炎症)的发现,以及 MAOs 作为分子生物标志物的作用及其在其他组织中的活性。

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